Abstract
Background: Niosomes are non-ionic surfactant vesicles used as drug carriers for encapsulating both hydrophobic and hydrophilic drugs. The aim of the present study was to prepare and characterize niosomes formulations for oral delivery of telmisartan and evaluated for its antihypertensive activity.
Method: Telmisartan loaded niosomes were prepared using thin film hydration method by varying the Span 60 and cholesterol at several molar ratios and characterized for vesicles size, polydispersity index, zeta potential, entrapment efficiency. The in vivo antihypertensive study of optimized formulation and molecular impact of angiotensin II type-1 receptor (AT1R) messenger Ribonucleic acid (mRNA) and protein expression on smooth vascular muscles of aorta was determined by real-time polymerase chain reaction (RT-PCR) and western blot analysis in Wistar albino rats.
Results: The optimized niosomes formulation NS6 presented vesicles size of 618.47 nm, polydispersity index of 0.86, with entrapment efficiency of 83.83% and possesses negative charge. In vivo study showed that the optimized formulation could reduce the systolic blood pressure in methyl prednisolone acetate induced hypertensive rats in close proximity to normal range of systolic blood pressure and maintain it over an extended period. In addition, telmisartan loaded niosomes treatment to hypertensive rats significantly attenuates the raised mRNA level and protein level of AT1R gene in comparison to hypertensive rats.
Conclusion: Results of present study confer the potential of developed niosomes as suitable carriers for improved oral delivery of telmisartan.
Keywords: Antihypertensive, niosomes, oral, telmisartan, western blot, mRNA.
Current Drug Delivery
Title:Sorbitane Monostearate and Cholesterol based Niosomes for Oral Delivery of Telmisartan
Volume: 15 Issue: 2
Author(s): Abdul Ahad*, Mohammad Raish, Fahad I. Al-Jenoobi and Abdullah M. Al-Mohizea
Affiliation:
- Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451,Saudi Arabia
Keywords: Antihypertensive, niosomes, oral, telmisartan, western blot, mRNA.
Abstract: Background: Niosomes are non-ionic surfactant vesicles used as drug carriers for encapsulating both hydrophobic and hydrophilic drugs. The aim of the present study was to prepare and characterize niosomes formulations for oral delivery of telmisartan and evaluated for its antihypertensive activity.
Method: Telmisartan loaded niosomes were prepared using thin film hydration method by varying the Span 60 and cholesterol at several molar ratios and characterized for vesicles size, polydispersity index, zeta potential, entrapment efficiency. The in vivo antihypertensive study of optimized formulation and molecular impact of angiotensin II type-1 receptor (AT1R) messenger Ribonucleic acid (mRNA) and protein expression on smooth vascular muscles of aorta was determined by real-time polymerase chain reaction (RT-PCR) and western blot analysis in Wistar albino rats.
Results: The optimized niosomes formulation NS6 presented vesicles size of 618.47 nm, polydispersity index of 0.86, with entrapment efficiency of 83.83% and possesses negative charge. In vivo study showed that the optimized formulation could reduce the systolic blood pressure in methyl prednisolone acetate induced hypertensive rats in close proximity to normal range of systolic blood pressure and maintain it over an extended period. In addition, telmisartan loaded niosomes treatment to hypertensive rats significantly attenuates the raised mRNA level and protein level of AT1R gene in comparison to hypertensive rats.
Conclusion: Results of present study confer the potential of developed niosomes as suitable carriers for improved oral delivery of telmisartan.
Export Options
About this article
Cite this article as:
Ahad Abdul *, Raish Mohammad , Al-Jenoobi I. Fahad and Al-Mohizea M. Abdullah , Sorbitane Monostearate and Cholesterol based Niosomes for Oral Delivery of Telmisartan, Current Drug Delivery 2018; 15 (2) . https://dx.doi.org/10.2174/1567201814666170518131934
DOI https://dx.doi.org/10.2174/1567201814666170518131934 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access of both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Nanotechnology Based Chemotherapy for the treatment of Head & Neck Cancer
The escalating recurrence rates observed in Head and Neck cancer, particularly within the chemo-therapeutically treated cohort (50-60%), can be attributed to the non-selective nature of current anticancer drug delivery modalities. In this context, nanotechnology-based drug delivery systems emerge as a promising avenue for achieving precise localization of therapeutic agents to ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Diabetes as a Negative Risk Factor for Abdominal Aortic Aneurysm – Does the Disease Aetiology or the Treatment Provide the Mechanism of Protection?
Current Vascular Pharmacology Differential ERK1/2 Signaling and Hypertrophic Response to Endothelin-1 in Cardiomyocytes from SHR and Wistar-Kyoto Rats: A Potential Target for Combination Therapy of Hypertension
Current Vascular Pharmacology Gender Differences in Metabolic Syndrome – A Key Research Issue
Endocrine, Metabolic & Immune Disorders - Drug Targets Role of Carbon Monoxide in Vascular Diseases
Current Pharmaceutical Biotechnology Self-care improvement after a pharmaceutical intervention in elderly type 2 diabetic patients
Current Diabetes Reviews Chronic Inflammatory Diseases and the Acute Respiratory Distress Syndrome (ARDS)
Current Pharmaceutical Design Oxidative Stress and its Clinical Consequences: Relationship between Diabetes and Cancer
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Novel Therapeutics for Diabetic Micro- and Macrovascular Complications
Current Medicinal Chemistry Transcatheter Aortic Valve Implantation versus Surgical Aortic Valve Replacement: Meta-Analysis of Clinical Outcomes and Cost-Effectiveness
Current Pharmaceutical Design The Osteopontin Tissue Level as a Breast Cancer Biomarker in Females After Mastectomy Measured by the Capillary Gel Electrophoresis Technique
Combinatorial Chemistry & High Throughput Screening Hunting for Peptide Substrates of Prolyl Oligopeptidase: Classical Versus Non-Classical Bioactive Peptides
CNS & Neurological Disorders - Drug Targets The Status of Disease Registries in the United States: Reflections
Applied Clinical Research, Clinical Trials and Regulatory Affairs Modulation of Potassium Channels as a Therapeutic Approach
Current Pharmaceutical Design The Prevalence, Morbidities, and Treatments of Insomnia
CNS & Neurological Disorders - Drug Targets Ethosomes as Novel Vesicular Carrier: An Overview of the Principle, Preparation and its Applications
Current Drug Delivery Angiotensin II Blockade and Renal Protection
Current Pharmaceutical Design The Effect of Local Alcohol Delivery in Reducing Intimal Hyperplasia Induced by Vascular Injury and the Clinical Implications
Vascular Disease Prevention (Discontinued) Cellular and Functional Effects of Insulin Based Therapies and Exercise on Endothelium
Current Pharmaceutical Design Vascular Calcification in Chronic Kidney Disease: Role of Disordered Mineral Metabolism
Current Pharmaceutical Design Polydeoxyribonucleotide (PDRN): A Safe Approach to Induce Therapeutic Angiogenesis in Peripheral Artery Occlusive Disease and in Diabetic Foot Ulcers
Cardiovascular & Hematological Agents in Medicinal Chemistry